Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 8,270 | 待询 | ||
50 mg | ¥ 12,800 | 待询 |
Cenicriviroc Mesylate 的其他形式现货产品:
产品描述 | Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity. |
靶点活性 | CCR5:0.29 nM, CCR2:5.9 nM, R5 HIV-1:0.024-0.08 nM (in PBMCs), R5 HIV-2:0.03-0.98 nM (in PBMCs) |
体外活性 | Migration of mouse monocytes in response to carbon tetrachloride (CCL2) is reduced following pre-treatment with Cenicriviroc Mesylate (CVC) at a concentration of 1 μM. Compare to untreated and unstimulated cells, the average fold change in migrating cells is 0.8±0.2 (p>0.05) and 0.7±0.4 (p>0.05) for CCL2-stimulated cells treated with Cenicriviroc Mesylate and unstimulated cells treated with Cenicriviroc Mesylate, respectively [1]. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC50 for Cenicriviroc Mesylate of 0.39 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC50 at >1000 nM, and Maximum percentages of inhibition at 33% and 4%, respectively [2]. |
体内活性 | Cenicriviroc Mesylate treatment leads to a dose-related decrease in monocyte/macrophage recruitment and achieving statistical significance at doses ≥20 mg/kg/day. Compare to the vehicle-control group, peritoneal lavage monocyte/macrophage counts are decreased by: 5.7%, 45.2%, 76.5% and 26.0% for Cenicriviroc Mesylate 5 twice daily (BID), Cenicriviroc Mesylate20 twice daily (BID), Cenicriviroc Mesylate100 BID, Cenicriviroc Mesylate 20 once-daily (QD), respectively. Exposure to Cenicriviroc Mesylate is dose-related and correlated with the decrease in monocyte/macrophage recruitment, with Cenicriviroc Mesylate appearing to be more effective when given BID versus QD, in line with the higher plasma concentrations achieved with BID dosing and the known short half-life in mice (~2 hours) [1]. |
别名 | TBR-652 Mesylate, TAK-652 Mesylate |
分子量 | 793.05 |
分子式 | C42H56N4O7S2 |
CAS No. | 497223-28-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (126.10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.261 mL | 6.3048 mL | 12.6095 mL | 31.5239 mL |
5 mM | 0.2522 mL | 1.261 mL | 2.5219 mL | 6.3048 mL | |
10 mM | 0.1261 mL | 0.6305 mL | 1.261 mL | 3.1524 mL | |
20 mM | 0.063 mL | 0.3152 mL | 0.6305 mL | 1.5762 mL | |
50 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
100 mM | 0.0126 mL | 0.063 mL | 0.1261 mL | 0.3152 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Cenicriviroc Mesylate 497223-28-6 Immunology/Inflammation Microbiology/Virology CCR TBR652 Mesylate TBR-652 Mesylate TAK-652 Mesylate TAK 652 Mesylate TBR 652 Mesylate TAK652 Mesylate Inhibitor inhibitor inhibit